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Lecithin carrier vesicles and methods of making the same

a technology of lecithin carrier and vesicles, which is applied in the field of lecithin carrier compositions and methods of making lecithin carrier compositions, can solve the problems of unfavorable active ingredient dispersion, so as to reduce the size of the membrane loaded lecithin vesicles and achieve high shear mixing

Inactive Publication Date: 2011-12-29
BIO UP MIMETIC TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0024]In some embodiments, this method further includes adding a stabilizing agent to the lecithin prior to hydration or to the lecithin vesicle prior to or after incorporation of the active ingredient. This method may also include, after incorpor

Problems solved by technology

However, these surfactant emulsions are often not stable, and the surfactant may be toxic or have undesired properties such as poor taste and / or the dispersion has cloudy appearance.
These properties render these emulsions inadequate for dispersion of an active ingredient for consumption.
However, high PC-content lecithin is costly to make, and methodologies requiring certain organic solvents render the composition not desirable for human consumption.

Method used

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  • Lecithin carrier vesicles and methods of making the same
  • Lecithin carrier vesicles and methods of making the same
  • Lecithin carrier vesicles and methods of making the same

Examples

Experimental program
Comparison scheme
Effect test

example 1-1

HLCV Dispersion of Fish Oil (Omega-3 Formulations)

[0095]20 g fish oil (EPAX 1050), 30 g lecithin (Cargill Lecigran), 0.5 g Vitamin E, and 4 ml ethanol were combined in a bottle. The mixture was mixed with heating to 65 C for about 60 minutes until the solution was homogeneous in appearance. This mixture was added to 250 ml of purified water that had been heated to 65° C. and was mixed for 5 minutes. 50 ml samples of this hydrated fish oil lecithin dispersion were combined with suitable volumes of ethanol to produce dispersions containing approximately 0, 10, 20, 30, 40 and 50% (v / v) ethanol. For the purpose of determining the amount of ethanol to add, the small volume already present (from the homogeneous lecithin phase) was ignored. Each dispersion in this series was homogenized (Niro Soavi NS 1001L homogenizer) at approximately 600 bar and 65° C. inlet temperature for 4 passes. Dispersions were then diluted in conditioned water to approximately 3 mg / ml fish oil. FIG. 1A shows a ph...

example 1-2

[0096]The HLCV Omega-3 dispersions were made as in Example 1-1, except 1.0 g of polysorbate 80 was added. A photograph of each of these Omega-3 formulations with polysorbate at 0, 10, 20, 30 40 and 50% ethanol is shown in FIG. 2A. Turbidity and particle size distribution data from dynamic light scattering for these formulations are shown in FIGS. 2B and 2C, respectively. As shown, the smallest volume weighted mean diameter, at 30% ethanol, with polysorbate is about 35 nm. FIG. 3 shows a side by side photograph of these Omega-3 formulations at 30% ethanol with and without polysorbate.

example 2

HLCV Dispersion of Essential Oils

[0097]10 g of Lecithin (Lecigran, Cargill or Ultralec, ADM) was hydrated with mixing in 100 ml distilled water and then homogenized at room temperature with 6 passes at approximately 400 bar through a Niro Soavi NS1001L homogenizer to form HLCVs. Polysorbate 80 was added with mixing at a weight ratio of lecithin:polysorbate of 5:1. The dispersion was then diluted to 200 ml using distilled water. The essential oils: thymol (0.7 g), eucalyptol (1.0 g), methyl salicylate (0.65 g) and menthol (0.46 g), were added and mixed to produce an essentially transparent aqueous dispersion of these essential oils. The resulting dispersion was filtered through a 0.2 micron filter. The transparent dispersion was diluted and sweeteners added to produce an ethanol-free essential oil mouthwash. A photograph of two samples of the essential oil dispersion are shown in FIG. 4A, one freshly prepared (t=0) and one stored at room temperature for 12 months (t=12 months). Resul...

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Abstract

A hydrated lecithin carrier vesicle composition includes a lecithin-derived membrane-forming lipid vesicle in conditioned water for incorporation of an active ingredient to form a dispersed composition. A method of making the hydrated lecithin carrier vesicle includes using lecithin having not more than about 80% w / w phosphatidylcholine in the presence of conditioned water.

Description

CROSS-REFERENCE TO RELATED APPLICATION(S)[0001]The present application claims priority to and the benefit of U.S. Provisional Application Ser. No. 61 / 357,959, filed on Jun. 23, 2010, the entire contents of which are incorporated herein by reference.TECHNICAL FIELD[0002]This application is directed to lecithin carrier compositions and methods of making lecithin carrier compositions.TECHNICAL BACKGROUND[0003]The dispersion and stabilization of active ingredients may be desirable in order to store and manipulate these desired compounds in aqueous environments. Commonly used methods for dispersion have included emulsions, in which droplets of the active ingredient are dispersed and stabilized by a surfactant, or by milling or shearing of the desired compound into nanoparticles and dispersing the nanoparticles into a surfactant. However, these surfactant emulsions are often not stable, and the surfactant may be toxic or have undesired properties such as poor taste and / or the dispersion h...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K38/43A61K31/56A61K38/13A61K31/05A23L1/222A61P31/00A61P31/14A23J7/00A23L3/3454A23L1/302A23D7/00A61K47/44A61K9/00A23L27/12A23L33/00A23L33/15C09K23/42
CPCA23D7/0053A61K9/127A23L1/0029A23L1/22016A23L1/222A23L1/3004A23L1/3006A23V2002/00A61K31/05A61K31/56A23D7/011A23V2200/224A23V2200/254A23V2250/1842A23V2250/1846A23P10/30A23L27/72A23L27/12A23L33/11A23L33/115A61K31/685A61K38/13A61K38/43A61P31/00A61P31/14A61K47/50A61K47/30A23L33/00A23L33/12A23L33/15A23D7/00A23J7/00A23L3/3454A61K9/00A61K47/44
Inventor ELEY, CRISPIN G. S.HODGSON, DONALD F.
Owner BIO UP MIMETIC TECH INC
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